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    Compounds for the Treatment of Neurological Disorders
    2.
    发明申请
    Compounds for the Treatment of Neurological Disorders 审中-公开
    用于治疗神经障碍的化合物

    公开(公告)号：US20140148432A1

    公开(公告)日：2014-05-29

    申请号：US14169833

    申请日：2014-01-31

    申请人： Ruppa Poornachary Kamalesh Babu ,  Scott James Myers

    发明人： Ruppa Poornachary Kamalesh Babu ,  Scott James Myers

    IPC分类号： A61K31/4709 ,  C07D211/22 ,  A61K31/445 ,  C07D401/12 ,  C07D401/14

    CPC分类号： A61K31/4709 ,  A61K31/4375 ,  A61K31/445 ,  C07D211/22 ,  C07D401/12 ,  C07D401/14

    摘要： Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activation, including neuropsychiatric disorders, neurodegenerative diorders and other neurologic diseases, disorders and conditions including stroke, brain injury, epilepsy, neuropsychiatric disorders, mood disorders, chronic pain and related conditions. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein Ar1 and Ar2 are independently substituted or unsubstituted aryl, heteroaryl or heterocycle; m, n, p and q are each independently 0, 1 or 2; A is a bond, CH2, CH═CH, C≡C, NR, O or S; Each R3 is independently selected from C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 haloalkyl, OH, O-alkyl, O-aryl, SH, S-alkyl, fluoro, chloro, bromo, iodo, nitro, or cyano; Q is selected from CH2, CHR, CR2, NH, NR, O and S; Each Y is independently CR2 or CR2CR2; each R is independently selected from H, OH or alkyl, in particular C1-4 alkyl; X is O, S, or CH2; and Z is OH, NR6R7, NR8SO2(C1-C6 alkyl), NR8C(O)NR6R7, NR8C(S)NR6R7, NR8CHO, NR8C(O)(C1-C6 alkyl), NR8C(O)O(C1-C6 alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole wherein each R6, R7 and R8 is independently H, C1-C6 alkyl or C6-C12 aralkyl; or Z comes together with Ar2 together to form a substituted or unsubstituted heterocyclic ring system with Ar2.

    摘要翻译： 本发明提供了治疗或预防某些神经系统疾病的化合物，药物组合物和方法，包括与NMDA受体活化相关的疾病，包括神经精神障碍，神经变性异常和其他神经疾病，疾病和病症，包括中风，脑损伤，癫痫，神经精神障碍， 情绪障碍，慢性疼痛及相关病症。 化合物为通式I，或其药学上可接受的盐，酯，前药或衍生物：其中Ar1和Ar2独立地为取代或未取代的芳基，杂芳基或杂环; m，n，p和q各自独立地为0,1或2; A是键，CH2，CH = CH，C≡C，NR，O或S; 每个R 3独立地选自C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6卤代烷基，OH，O-烷基，O-芳基，SH，S-烷基，氟，氯，溴，碘，硝基或氰基; Q选自CH 2，CHR，CR 2，NH，NR，O和S; 每个Y独立地为CR2或CR2CR2; 每个R独立地选自H，OH或烷基，特别是C 1-4烷基; X是O，S或CH 2; 并且Z是OH，NR6R7，NR8SO2（C1-C6烷基），NR8C（O）NR6R7，NR8C（S）NR6R7，NR8CHO，NR8C（O）（C1-C6烷基），NR8C（O） ），NR8-二氢噻唑或NR8-二氢咪唑，其中每个R 6，R 7和R 8独立地为H，C 1 -C 6烷基或C 6 -C 12芳烷基; 或Z一起与Ar 2一起形成具有Ar 2的取代或未取代的杂环系统。